Legality and use of sublingual (under the tongue) CBD

What is CBD and what is it for?

Cannabidiol or CBD is one of the main active ingredients of the Cannabis plant, nowadays known worldwide for its therapeutic properties recognised by the WHO. The importance of CBD in the therapeutic field is due to its low level of toxicity compared to other drugs, the fact that it does not cause tolerance or dependence and its multiple medicinal properties, among which analgesic, anti-inflammatory, neuroprotective and relaxing properties on a physical and mental level stand out. (1-2-3-4)

CBD legislation: key points for the UN to recognise its therapeutic properties

In 2017 the WHO recommended the declassification of CBD as a narcotic and controlled or prohibited substance, due to its lack of toxicity and danger of abuse (1).

Following this recommendation, many countries modified their laws, allowing the use of CBD without many limitations until 2019, the year in which the European Commission declared Cannabis extracts as "novel food", only allowing its use, production and registration as a cosmetic and prohibiting its food use (in Europe).

However, in 2020 the UN declassified all Cannabis compounds from schedule IV of the Single Convention on Narcotic Substances, stating that CBD is a safe substance to be considered as food. (12)

So in the very near future, we should see a classification of CBD at both food and pharmaceutical level.

European regulatory processes aside, the safety of CBD for human consumption is very clear, for several reasons:

• There are many countries that allow it to be marketed as a food and there are studies on its safety and guidelines on its production (13)
• There are many countries that have approved a medical Cannabis programme in their health care system
• Major pharmaceutical companies have been studying and developing cannabinoid medicines for internal use for many years, in particular via the sublingual route (11).

What is the most effective method of using CBD?

There are different ways of taking CBD, each with its own peculiarities:

• Inhalation: through the inhaled route the effect appears immediately and at its maximum potency, gradually reducing until it disappears after 2 hours. The most appropriate and effective way would be vaporisation, which ensures high bioavailability (35%-50%) compared to combustion (30%), which also entails risks and damage to the body's health. (5-6)
• Ingestion: through the ingested route, the effect appears after 1-2 hours and is maintained for 8-10 hours in an irregular manner, as it depends on the metabolism of each person. Due to the passage through the digestive system, ingestion ensures low bioavailability (4%-12%), as well as facilitating drug-drug interactions (7).
• Sublingual: the effect appears after 20-30 minutes via the sublingual route and remains stable for approximately 6 hours. By taking CBD sublingually correctly, the passage of CBD through the digestive system is avoided and its bioavailability is increased (15%-35%), in addition to avoiding possible drug interactions and ensuring the stability of the effect (8-9). For these reasons, the sublingual route is the most effective way to use CBD internally.
• External use: the topical route concentrates the effect in the area of application for 2-3 hours, unlike transdermal use, which allows for a systemic effect.

How is sublingual CBD taken in regulated countries?

Due to the aforementioned advantages, the sublingual route is the most suitable way to use CBD to deal with physical and psychological problems that manifest themselves in a stable and/or chronic form, as it would ensure a continuous and stable effect.

Through this route, CBD is absorbed through the sublingual mucosa and reaches the bloodstream quickly, avoiding first-pass metabolism and increasing bioavailability compared to ingestion (10).

Sublingual products are oils with different concentrations of CBD (minimum 5%), which can be administered by dropper or spray.

To take sublingually, the drops or sprays should be placed under the tongue and held under the tongue for at least 60-90 seconds without swallowing.

Tips: You should get used to sublingual injections, as the first few times you will notice an increase in saliva in your mouth, which will be a little uncomfortable to hold for more than a minute. If you have accumulated a lot of saliva, it is possible to spread the liquid in the mouth before swallowing so that it stays in the mouth for longer.

How long is CBD left under the tongue?

Each person has a different organism and a different sensitivity to substances, so there is no standardised dosage of CBD for different types of people or types of pathology. In addition, Cannabis has a biphasic effect, so to obtain the best benefits it is necessary to use the right dose for each person, as an excessive dose could facilitate the appearance of some side effects (such as nausea and headache) and even diminish the benefits. For these reasons, it is always advisable to consult a specialised health professional who can provide appropriate advice and follow-up.

In general, it is advisable to start with low to medium concentration products (5%-10%), beginning with one drop per intake and gradually increasing every 2 or 3 days according to the sensations perceived until the effects appear.

How many CBD drops are taken?

To optimise sublingual absorption, it is advisable to use as few drops as possible, as sublingual space is limited. For this reason it is very important not to exceed the number of drops in each dose, using a maximum of 6-7 drops.

If I am taking 6-7 drops and want to increase the dose, how do I proceed?

• The first option is to use a more concentrated oil in order to reduce the number of drops (6 drops at 5% corresponds to 3 drops at 10%, 2 at 15% or 1 at 30%).
• The second option is to use the same oil and divide the intake in two consecutive moments: for example, take 4-5 drops initially and 2-3 minutes later the others.

How long does it take for CBD to take effect?

Through the sublingual route, the effect lasts approximately 6 hours, therefore, as a continuous effect is required, it can be taken 3 times a day: morning, afternoon and evening.

This is the case for chronic problems, such as chronic pain and inflammation or psycho-physical problems such as anxiety and excessive stress.

The effect of sublingual CBD can vary in duration, so in some people it can last 4-5 hours and in others up to 12 hours. In these cases, through monitoring it is possible to increase or decrease the doses as needed. In addition, depending on the symptoms of each person, it is possible to reduce the doses at the times of the day when the symptoms appear.

Which CBD product is right for me?

If you want to use CBD continuously, to try to alleviate stable or chronic problems such as pain, inflammation, emotional problems and states of stress and anxiety, in the United States and / or Canada the sublingual route is recommended (not regulated in Spain), using a low or medium concentration oil under the advice and monitoring of a specialised health professional.

To deal with acute problems or to reinforce the effect at specific times, it is possible to complement the treatment using the inhaled route, as in the case of acute pain or anxiety and panic attacks, dosing according to need.

In case of skin problems or joint and muscle problems, it is also possible to complement the treatment with the topical route, to concentrate the action of CBD in the area of application.

Bibliography:

1. CANNABIDIOL (CBD) Pre-Review Report Agenda Item 5.2 Expert Committee on Drug Dependence Thirty-ninth Meeting Geneva, 6-10 November 2017 
2. CANNABIDIOL (CBD) Critical Review Report Expert Committee on Drug Dependence Fortieth Meeting Geneva, 4-7 June 2018 
3. Bergamaschi MM, Queiroz RH, Zuardi AW, Crippa JA. Safety and side effects of cannabidiol, a Cannabis sativa constituent. Curr Drug Saf. 2011 Sep 1;6(4):237-49 
4. Iffland K, Grotenhermen F. An Update on Safety and Side Effects of Cannabidiol: A Review of Clinical Data and Relevant Animal Studies. Cannabis Cannabinoid Res. 2017 Jun 1;2(1):139-154 
5. McGilveray I. J. (2005). Pharmacokinetics of cannabinoids. Pain research & management, 10 Suppl A, 15A–22A.
6. Lanz, C., Mattsson, J., Soydaner, U., & Brenneisen, R. (2016). Medicinal Cannabis: In Vitro Validation of Vaporizers for the Smoke-Free Inhalation of Cannabis. PloS one, 11(1).
7. Chayasirisobhon S. (2020). Mechanisms of Action and Pharmacokinetics of Cannabis. The Permanente journal, 25, 1–3.
8. Mechoulam, R., Parker, L. A., & Gallily, R. (2002). Cannabidiol: an overview of some pharmacological aspects. Journal of clinical pharmacology, 42(S1), 11S–19S. 
9. Narang, N.C., Sharma, J., & Baba, S. (2011). SUBLINGUAL MUCOSA AS A ROUTE FOR SYSTEMIC DRUG DELIVERY. 
10. Hosseini, A., McLachlan, A. J., & Lickliter, J. D. (2021). A phase I trial of the safety, tolerability and pharmacokinetics of cannabidiol administered as single-dose oil solution and single and multiple doses of a sublingual wafer in healthy volunteers. British journal of clinical pharmacology, 87(4), 2070–2077.
11. Cannabis-based medicines--GW pharmaceuticals: high CBD, high THC, medicinal cannabis--GW pharmaceuticals, THC:CBD. (2003). Drugs in R&D, 4(5), 306–309.
12. https://www.emcdda.europa.eu/news/2020/cannabidiol-cbd-is-not-considered-a-narcotic-drug-under-european-law_en
13. Walker, L. A., Koturbash, I., Kingston, R., ElSohly, M. A., Yates, C. R., Gurley, B. J., & Khan, I. (2020). Cannabidiol (CBD) in Dietary Supplements: Perspectives on Science, Safety, and Potential Regulatory Approaches. Journal of dietary supplements, 17(5), 493–502.